Inhibition of human polymorphonuclear leukocyte cell responses by ibuprofen

• Published in: Journal of pharmaceutical sciences Vol. 73; no. 10; p. 1403
• Main Authors: Maderazo, E G, Breaux, S P, Woronick, C L
• Format: Journal Article
• Language: English
• Published: United States 01.10.1984
• Subjects: Blood Bactericidal Activity; Cell Aggregation - drug effects; Cell Movement - drug effects; Chemotactic Factors - pharmacology; Complement C5 - pharmacology; Complement C5a; Female; Humans; Ibuprofen - pharmacology; In Vitro Techniques; Lysosomes - enzymology; Male; Neutrophils - cytology; Neutrophils - drug effects; Nitroblue Tetrazolium - metabolism; Staphylococcus aureus - physiology
• ISSN: 0022-3549
• DOI: 10.1002/jps.2600731020

The stimulation of cell swelling, cell aggregation, polymorphonuclear leukocyte locomotion, and lysosomal enzyme release in response to chemoattractant were all inhibited by ibuprofen, a nonsteroidal anti-inflammatory agent. The dosages needed to induce 50% inhibition (ID50) were 5.9, 7.6, 60, and 95 micrograms/mL, respectively. Aside from the differences in ID50, there was also a difference in the degree of maximum inhibition (Imax) of the complement C5a-stimulated responses observed, so that at achievable serum drug concentrations of 20-50 micrograms/mL, inhibition of 67-78% for cell swelling, 69-82% for cell aggregation, 20-35% for migration response, and 17-38% for lysosomal enzyme release were demonstrated. Also observed were a minor stimulatory effect on nitroblue tetrazolium reduction and an inhibitory effect on the ability to kill Staphylococcus aureus, but only at very high concentrations (approximately 2 mg/mL).